Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
Type:
Grant
Filed:
May 4, 2018
Date of Patent:
February 22, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Niels P. Ryde, Peter Snyder, Wei Liu, David M. Slifer
Abstract: The invention provides compositions, methods and treatment regimens for treating cancer comprising periodic subcutaneous administration of the fusion protein of SEQ ID NO:1 to a cancer patient resulting in enhanced activation of CD8+ T-cells with minimal effects on regulatory T cell (Treg) expansion and providing enhanced anti-tumor efficacy while also mitigating T cell inactivation/exhaustion.
Type:
Grant
Filed:
June 10, 2020
Date of Patent:
February 15, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Heather C. Losey, Jared Lopes, Lei Sun, Raymond J. Winquist
Abstract: The invention provides compositions and methods of treating cancer in a patient with a combination therapy comprising a fusion protein of SEQ ID NO: 1 in combination with an immune checkpoint inhibitor. Preferably the patient has failed to achieve complete or partial response with prior or ongoing treatment with an immune checkpoint inhibitor.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
February 15, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Heather C. Losey, Jared Lopes, Raymond J. Winquist
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.
Type:
Grant
Filed:
August 7, 2020
Date of Patent:
January 25, 2022
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.
Type:
Grant
Filed:
June 17, 2020
Date of Patent:
October 26, 2021
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Philip Cresswell, Magali Hickey, Kristopher Perkin, Greg Smith, Elaine Liversidge, Brian Steinberg, David Manser, Tarek Zeidan
Abstract: The present invention relates to a pharmaceutical composition that provides long-term stability of a hydrolytically labile antipsychotic agent
Type:
Grant
Filed:
March 30, 2020
Date of Patent:
August 24, 2021
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Jason M. Perry, Daniel R. Deaver, Magali B. Hickey, Julius F. Remenar, Jennifer Vandiver, Michael J. Palmieri, Jr., Zhengzheng Pan
Abstract: Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
Type:
Grant
Filed:
October 8, 2019
Date of Patent:
April 13, 2021
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Wilfredo Morales, Tarek A. Zeidan, Renato A. Chiarella, Steven G. Wright, Jason M. Perry
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
November 5, 2019
Date of Patent:
April 13, 2021
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri Theodore Moustakas, Thomas Andrew Wynn, Todd Bosanac
Abstract: Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.
Type:
Grant
Filed:
June 29, 2018
Date of Patent:
December 1, 2020
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Philip Cresswell, Magali Hickey, Kristopher Perkin, Greg Smith, Elaine Liversidge, Brian Steinberg, David Manser, Tarek Zeidan
Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
Type:
Grant
Filed:
May 29, 2019
Date of Patent:
November 3, 2020
Assignee:
ALKERMES PHARMA IRELAND LIMITED
Inventors:
Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
Abstract: The present invention relates to pharmaceutical compositions comprising a compound of Formula (I) that are useful for the intramuscular delivery of antipsychotic drugs using rapid injection rates.
Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ C max ? ( BUP ) / EC 50 ] [ C max ? ( ANTAGONIST ) / IC 50 ] .
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
July 11, 2019
Date of Patent:
October 20, 2020
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri T. Moustakas, Thomas Andrew Wynn, Todd Bosanac
Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
Type:
Grant
Filed:
July 11, 2019
Date of Patent:
October 13, 2020
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri T. Moustakas, Thomas Andrew Wynn, Todd Bosanac